Helisch A, Schirrmacher E, Thews O, Schirrmacher R, Buchholz H G, Dillenburg W, Höhnemann S, Tillmanns J, Wessler I, Buhl R, Rösch F, Bartenstein P
Department of Nuclear Medicine, University Hospital, Langenbeckstrasse 1, 55101 Mainz, Germany.
Eur J Nucl Med Mol Imaging. 2005 Nov;32(11):1324-8. doi: 10.1007/s00259-005-1914-9. Epub 2005 Aug 31.
The new beta2 radioligand (R,R)(S,S) 5-(2-(2-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylethylamino)-1-hydroxyethyl)-benzene-1,3-diol ([18F]FE-fenoterol; [18F]FEFE), a fluoroethylated derivative of racemic fenoterol, was evaluated in vivo and ex vivo using a guinea pig model.
Dynamic PET studies over 60 min with [(18)F]FEFE were performed in nine Hartley guinea pigs in which a baseline (group 1, n=3), a predose (group 2, n=3; 2 mg/kg fenoterol 5 min prior to injection of [18F]FEFE) or a displacement study (group 3, n=3; 2 mg/kg fenoterol 5 min post injection of [18F]FEFE) was conducted.
In all animal groups, the lungs could be visualised and semi-quantified separately by calculating uptake ratios to non-specific binding in the neck area. Premedication with non-radioactive fenoterol and displacement tests showed significant reduction of lung uptake, by 94% and 76%, respectively.
These data demonstrate specific binding of the new radioligand to the pulmonary beta2-receptors in accordance with ex vivo measurements. Therefore, [18F]FEFE seems to be suitable for the in vivo visualisation and quantification of the pulmonary beta2-receptor binding in this animal model.
新型β2放射性配体（R,R）（S,S）5-（2-（2-[4-（2-[18F]氟乙氧基）苯基]-1-甲基乙氨基）-1-羟乙基）-苯-1,3-二醇（[18F]FE-非诺特罗；[18F]FEFE），一种消旋非诺特罗的氟乙基化衍生物，使用豚鼠模型进行体内和体外评估。
对9只哈特利豚鼠进行了60分钟的[(18)F]FEFE动态PET研究，其中进行了基线研究（第1组，n = 3）、给药前研究（第2组，n = 3；在注射[18F]FEFE前5分钟给予2 mg/kg非诺特罗）或置换研究（第3组，n = 3；在注射[18F]FEFE后5分钟给予2 mg/kg非诺特罗）。
在所有动物组中，通过计算与颈部区域非特异性结合的摄取率，可以分别对肺部进行可视化和半定量分析。用非放射性非诺特罗进行预处理和置换试验显示肺部摄取分别显著降低了94%和76%。
这些数据表明新型放射性配体与肺β2受体存在特异性结合，与体外测量结果一致。因此，[18F]FEFE似乎适用于该动物模型中肺β2受体结合的体内可视化和定量分析。
